1,3,4-oxadiazole derivatives as DGAT1 inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C548S143000

Reexamination Certificate

active

08003676

ABSTRACT:
Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided,wherein:n is 1, 2 or 3 and each R is independently selected from fluoro, chloro, cyano, methyl, ethyl, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy and difluoromethoxy; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.

REFERENCES:
patent: 3245989 (1966-04-01), Palazzo
patent: 4983731 (1991-01-01), Wagner et al.
patent: 5491172 (1996-02-01), Lee et al.
patent: 6608185 (2003-08-01), Omura et al.
patent: 6624185 (2003-09-01), Glombik et al.
patent: 7138414 (2006-11-01), Schoenafinger et al.
patent: 7453010 (2008-11-01), Bovy et al.
patent: 7749997 (2010-07-01), Birch et al.
patent: 7795283 (2010-09-01), Birch et al.
patent: 2002/0183384 (2002-12-01), Cornicelli et al.
patent: 2003/0072757 (2003-04-01), Farese et al.
patent: 2004/0102432 (2004-05-01), Sanganee et al.
patent: 2005/0070545 (2005-03-01), Fox et al.
patent: 2007/0123504 (2007-05-01), Bolin et al.
patent: 2007/0155832 (2007-07-01), Haeberlein et al.
patent: 2007/0249620 (2007-10-01), Kurata et al.
patent: 2008/0090876 (2008-04-01), Cheng et al.
patent: 2008/0096874 (2008-04-01), Birch et al.
patent: 2008/0306059 (2008-12-01), Birch et al.
patent: 2008/0312282 (2008-12-01), Judd et al.
patent: 2009/0048258 (2009-02-01), Ogino et al.
patent: 2009/0093497 (2009-04-01), Bolin et al.
patent: 2009/0197926 (2009-08-01), Birch et al.
patent: 2009/0209602 (2009-08-01), Butlin et al.
patent: 2009/0215779 (2009-08-01), Butlin et al.
patent: 2009/0275620 (2009-11-01), Butlin et al.
patent: 2009/0298853 (2009-12-01), Bauer et al.
patent: 2010/0029727 (2010-02-01), Johnstone et al.
patent: 2010/0160397 (2010-06-01), Birch et al.
patent: 2010/0173958 (2010-07-01), Bennett et al.
patent: 2010/0184813 (2010-07-01), Birch et al.
patent: 2010/0311737 (2010-12-01), Birch et al.
patent: 10223273 (2003-12-01), None
patent: 1236468 (2002-09-01), None
patent: 1541563 (2005-06-01), None
patent: 1661889 (2006-05-01), None
patent: 1760071 (2007-03-01), None
patent: 2002284741 (2002-03-01), None
patent: 2004/067635 (2004-03-01), None
patent: 2005/206492 (2005-08-01), None
patent: 2007/131584 (2007-05-01), None
patent: 2007/191471 (2007-08-01), None
patent: 2010132590 (2010-06-01), None
patent: WO 94/26702 (1994-11-01), None
patent: WO 00/58491 (2000-10-01), None
patent: WO 00/72832 (2000-12-01), None
patent: WO 02/20484 (2002-03-01), None
patent: WO 03/099772 (2003-12-01), None
patent: WO 2004/007455 (2004-01-01), None
patent: WO 2004/017920 (2004-03-01), None
patent: WO 2004/032882 (2004-04-01), None
patent: WO 2004/047755 (2004-06-01), None
patent: WO 2004/062601 (2004-07-01), None
patent: WO 2004/089927 (2004-10-01), None
patent: WO 2004/100881 (2004-11-01), None
patent: WO 2004/110350 (2004-12-01), None
patent: WO 2005/013907 (2005-02-01), None
patent: WO 2005/027892 (2005-03-01), None
patent: WO 2005/037826 (2005-04-01), None
patent: WO 2005/044250 (2005-05-01), None
patent: WO 2005/046670 (2005-05-01), None
patent: WO 2005/072740 (2005-08-01), None
patent: WO 2006/004200 (2006-01-01), None
patent: WO 2006/019020 (2006-02-01), None
patent: WO 2006/044775 (2006-04-01), None
patent: WO 2006/054370 (2006-05-01), None
patent: WO 2006/064189 (2006-06-01), None
patent: WO 2006/082010 (2006-08-01), None
patent: WO 2006/082952 (2006-08-01), None
patent: WO 2006/113919 (2006-10-01), None
patent: WO 2006/120125 (2006-11-01), None
patent: WO 2006/134317 (2006-12-01), None
patent: WO 2007/007588 (2007-01-01), None
patent: WO 2007/016538 (2007-02-01), None
patent: WO 2007/060140 (2007-05-01), None
patent: WO 2007/071966 (2007-06-01), None
patent: WO 2007/074753 (2007-07-01), None
patent: WO 2007/124337 (2007-11-01), None
patent: WO 2007/126957 (2007-11-01), None
patent: WO 2007/137103 (2007-11-01), None
patent: WO 2007/137107 (2007-11-01), None
patent: WO 2007/138304 (2007-12-01), None
patent: WO 2007/138311 (2007-12-01), None
patent: WO 2007/141502 (2007-12-01), None
patent: WO 2007/141517 (2007-12-01), None
patent: WO 2007/141538 (2007-12-01), None
patent: WO 2007/141545 (2007-12-01), None
patent: WO 2007/144571 (2007-12-01), None
patent: WO 2008/011130 (2008-01-01), None
patent: WO 2008/011131 (2008-01-01), None
patent: WO 2008/039007 (2008-04-01), None
patent: WO 2008/039008 (2008-04-01), None
patent: WO 2008/040651 (2008-04-01), None
patent: WO 2008/046216 (2008-04-01), None
patent: WO 2008/048991 (2008-04-01), None
patent: WO 2008/058402 (2008-05-01), None
patent: WO 2008/067257 (2008-06-01), None
patent: WO 2008/073865 (2008-06-01), None
patent: WO 2008/099221 (2008-08-01), None
patent: WO 2008/129319 (2008-10-01), None
patent: WO 2008/134690 (2008-11-01), None
patent: WO 2008/134693 (2008-11-01), None
patent: WO 2008/141976 (2008-11-01), None
patent: WO 2008/148840 (2008-12-01), None
patent: WO 2008/148849 (2008-12-01), None
patent: WO 2008/148851 (2008-12-01), None
patent: WO 2008/148868 (2008-12-01), None
patent: WO 2008/154642 (2008-12-01), None
patent: WO 2009/009041 (2009-01-01), None
patent: WO 2009/011285 (2009-01-01), None
patent: WO 2009/016462 (2009-02-01), None
patent: WO 2009/024821 (2009-02-01), None
patent: WO 2009/037222 (2009-03-01), None
patent: WO 2009/040410 (2009-04-01), None
patent: WO 2009/071483 (2009-06-01), None
patent: WO 2009/081195 (2009-07-01), None
patent: WO 2009/112445 (2009-09-01), None
patent: WO 2009/119534 (2009-10-01), None
patent: WO 2009/126624 (2009-10-01), None
patent: WO 2009/126861 (2009-10-01), None
patent: WO 2009/137938 (2009-11-01), None
patent: WO 2010/007046 (2010-01-01), None
patent: WO 2010/017040 (2010-02-01), None
patent: WO 2010/023609 (2010-03-01), None
patent: WO 2010/048149 (2010-04-01), None
patent: WO 2010/056496 (2010-05-01), None
patent: WO 2010/056506 (2010-05-01), None
patent: WO 2010/059602 (2010-05-01), None
patent: WO 2010/059606 (2010-05-01), None
patent: WO 2010/059611 (2010-05-01), None
patent: WO 2010/065310 (2010-06-01), None
patent: WO 2010/070343 (2010-06-01), None
patent: WO 2010/077861 (2010-07-01), None
patent: WO 2010/083280 (2010-07-01), None
patent: WO 2010/084979 (2010-07-01), None
patent: WO 2010/086820 (2010-08-01), None
patent: WO 2010/089685 (2010-08-01), None
patent: WO 2010/089686 (2010-08-01), None
patent: WO 2010/091041 (2010-08-01), None
patent: WO 2010/095766 (2010-08-01), None
patent: WO 2010/107765 (2010-09-01), None
patent: WO 2010/107768 (2010-09-01), None
patent: WO 2010/108051 (2010-09-01), None
patent: WO 2010/122968 (2010-10-01), None
Adcock et al., “Electronic effect of the tricyanomethyl group by carbon-13 and fluorine-19 NMR: nature of aryl fluorine-19 NMR polar field effects in the benzene and naphthalene ring systems” Journal of Organic Chemistry 44 (17): 3004-3017 (1979).
Anderson et al. “Identification of a Form of Acyl-CoA:Cholesterol Acyltransferase Specific to Liver and Intestine in Nonhuman Primates” J Biol Chem 273(41):26747-26754 (1998).
Birch et al. “Discovery of a Potent, Selective, and Orally Efficacious Pyrimidinooxazinyl Bicyclooctaneacetic Acid Diacylglycerol Acyltransferase-1 Inhibitor” J. Med. Chem. 52(6):1558-1568 (2009).
Brown and Goldstein “Lipoprotein metabolism in the macrophage: implications for cholesterol deposition in atherosclerosis” Annu Rev Biochem. 52:223-261 (1983).
Burnett and Huff “Avasimibe Pfizer” Curr Opin Investig Drugs 3(9):1328-1333 (2002).
CAPLUS RN 404032-15-1, retrieved from CAPLUS on Jul. 17, 2009.
Cases et al. “ACAT-2, A Second Mammalian Acyl-CoA:Cholesterol Acyltransferase” J Biol Chem 273(41):26755-26764 (1998).
Cases et al. “Cloning of DGAT2, a Second Mammalian Diacylglycerol Acyltransferase, and Related Family Members” J. Biol. Chem. 276(42):38870-38876 (2001).
Cases et al. “Identification of a gene encoding an acyl CoA:diacylglycerol acyltransferase, a key enzyme in triacylglycerol synthesis” Proc Natl Acad Sci U S A. 95(22):13018-13023 (1998).
Chang et al. “

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

1,3,4-oxadiazole derivatives as DGAT1 inhibitors does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with 1,3,4-oxadiazole derivatives as DGAT1 inhibitors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 1,3,4-oxadiazole derivatives as DGAT1 inhibitors will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-2724878

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.